Pyrrolo-pyrimidones: a novel class of MK2 inhibitors with potent cellular activity |
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| Authors: | Schlapbach Achim Feifel Roland Hawtin Stuart Heng Richard Koch Guido Moebitz Henrik Revesz Laszlo Scheufler Clemens Velcicky Juraj Waelchli Rudolf Huppertz Christine |
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| Institution: | Novartis Institutes for BioMedical Research, global Discovery Chemistry, WSJ-88.508, CH-4002 Basel, Switzerland. achim.schlapbach@novartis.com |
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| Abstract: | Pyrrolo-pyrimidones of the general structure 1 were synthesized and evaluated for their potential as MK2 inhibitors. Potent derivatives were discovered which inhibit MK2 in the nanomolar range and show potent inhibition of cytokine release from LPS-stimulated monocytes. These derivatives were shown to inhibit phosphorylation of hsp27, a downstream target of MK2 and are modestly selective in a panel of 28 kinases. |
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